New antibacterial compounds and biological applications thereofThe invention relates to compounds of formulae (Ia), (Ib) or (Ic) wherein, -A1 and A2, identical or different, are H, (C1-C6) alkyl, (C1-C6) fluoroalkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, (C1-C6) alkyl-ORa, (C1-C6) alkyl-SRa, (C1-C6) alkyl-NRaRb, ORa, SRa, NRaRb, or CORa; - A3 is H, OH or form a carbonyl with A4; -A4 is H, OH or form a carbonyl with A3; -A5 is H, CRaRbOH, F, OH or forms a double bond with X in the case where X is CH; -A6 is H or F; -X is CH2, CHF, CF2, CHOH, O, S, NRa or a simple bond, or X is CH in the case where A5 forms with X a double bond; -Y is P(O) (ORa) (ORb) or P (O) (ORa) (NRaRb); -V is O or S; -A7 is H, (C1-C6) alkyl, (C1-C6) fluoroalkyl, (C2-C6) alkenyl, (C2-C6) alkynyl or (C1-C6) alkyl-ORa; -A8 is OH or H, -Ra and Rb, identical or different, are H, (C1-C6) alkyl, (C1-C6) fluoroalkyl, (C1-C6) alkyl-OH or (C1-C6) alkyl-O-(C1- C6) alkyl; and their addition salts thereof with acids and bases, their preparation and their use in the antibacterial prevention and therapy, used alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity.There is the compound of general formula (i),wherein,-a 1and a 2identical or different, it is h, (c 1-c 6) alkyl, fluoro (c 1-c 6) alkyl, (c 2-c 6) thiazolinyl, (c 2-c 6) alkynyl, (c 1-c 6) alkyl-or a, (c 1-c 6) alkyl-sr a, (c 1-c 6) alkyl-nr ar b, or a, sr a, nr ar bor cor a; -a 3for h, oh, or a 3with a 4form carbonyl; -a 4for h, oh, or a 4with a 3form carbonyl; -a 5for h, cr ar boh, f, oh, or when x is ch, a 5double bond is become with x-shaped; -a 6for h or f; -x is ch 2, chf, cf 2, choh, o, s, nr aor singly-bound, or work as a 5when becoming double bond with x-shaped, x is ch; -y is p (o) (or a) (or b) or p (o) (or a) (nr ar b); -v is o or s;-a 7for h, (c 1-c 6) alkyl, fluoro (c 1-c 6) alkyl, (c 2-c 6) thiazolinyl, (c 2-c 6) alkynyl or (c 1-c 6) alkyl-or a; -a 8for oh or h; -r aand r bidentical or different, it is selected from h, (c 1-c 6) alkyl, fluoro (c 1-c 6) alkyl, (c 1-c 6) alkyl-oh and (c 1-c 6) alkyl-o-(c 1-c 6) alkyl; described compound is pure diastereomer or the form of mixtures of diastereomer, and with the ring-type hemiketal of the compound of carbonyl and hydroxyl or cyclic hemiacetal form,and the additive salt of they and bronsted lowry acids and bases bronsted lowry.
신규 항균 화합물 및 이들의 생물학적 용도본 발명은 하기의 화학식(I)의 화합물; 및 이들의 산 및 염기와의 부가염에 관한 것이며:화학식(I) - 동일하거나 다른, A1 및 A2는 H, (C1-C6)알킬((C1-C6)alkyl), (C1-C6)플루오로알킬((C1-C6)fluoroalkyl), (C2-C6)알케닐((C2-C6)alkenyl), (C2-C6)알키닐((C2-C6)alkynyl), (C1-C6)알킬-ORa((C1-C6)alkyl-ORa), (C1-C6)알킬-SRa((C1-C6)alkyl-SRa), (C1-C6)알킬-NRaRb((C1-C6)alkyl-NRaRb), ORa, SRa, NRaRb, 또는 CORa이며, - A3는 H, OH 이거나 A4와 카르보닐기(carbonyl)를 형성하고; - A4는 H, OH 이거나 상기 A3와 카르보닐기(carbonyl)를 형성하며; - A5는 CRaRbOH, F, OH 이거나 X가 CH인 경우에 X와 이중 결합을 형성하고; - A6는 H 또는 F이며; - X는 CH2, CHF, CF2, CHOH, O, S, NRa 또는 단일 결합이거나, X는 A5가 X와 이중 결합을 형성하는 경우 CH이고; - Y는 P(O)(ORa)(ORb) 또는 P(O)(ORa)(NRaRb)이며; - V는 O 또는 S이고; - A7는 H, (C1-C6)알킬((C1-C6)alkyl), (C1-C6)플루오로알킬((C1-C6)fluoroalkyl), (C2-C6)알케닐((C2-C6)alkenyl), (C2-C6)알키닐((C2-C6)alkynyl) 또는 (C1-C6)알킬-ORa((C1-C6)alkyl-ORa)이며; - A8는 OH 또는 H이고; - 동일하거나 다른, Ra 및 Rb는 H, (C1-C6)알킬((C1-C6)alkyl), (C1-C6)플루오로알킬((C1-C6)fluoroalkyl), (C1-C6)알킬-OH((C1-C6)alkyl-OH) 및 (C1-C6)알킬-O-(C1-C6)알킬((C1-C6)alkyl-O-(C1-C6)alkyl)으로 이루어진 그룹으로부터 선택되며; 항균성 예방 및 치료에서 이들이 제조되고 이용되며, 항균제(antibacterials) 또는 항바이러스제(antivirulence agents) 또는 선천적 면역을 강화시키는 약물과 결합하여 또는 단독으로 이용된다. 화학식(I)을 가지는 화합물 및 이들의 산 및 염기와의 부가염으로서, [이미지]화학식(I)- 동일하거나 다른, A1 및 A2는 H, (C1-C6)알킬((C1-C6)alkyl), (C1-C6)플루오로알킬((C1-C6)fluoroalkyl), (C2-C6)알케닐((C2-C6)alkenyl), (C2-C6)알키닐((C2-C6)alkynyl), (C1-C6)알킬-ORa((C1-C6)alkyl-ORa), (C1-C6)알킬-SRa((C1-C6)alkyl-SRa), (C1-C6)알킬-NRaRb((C1-C6)alkyl-NRaRb), ORa, SRa, NRaRb, 또는 CORa이며,- A3는 H, OH 이거나 A4와 카르보닐기(carbonyl)를 형성하고;- A4는 H, OH 이거나 상기 A3와 카르보닐기(carbonyl)를 형성하며;- A5는 CRaRbOH, F, OH 이거나 X가 CH인 경우에 X와 이중 결합을 형성하고;- A6는 H 또는 F이며;- X는 CH2, CHF, CF2, CHOH, O, S, NRa 또는 단일 결합이거나, X는 A5가 X와 이중 결합을 형성하는 경우 CH이고;- Y는 P(O)(ORa)(ORb) 또는 P(O)(ORa)(NRaRb)이며;- V는 O 또는 S이고;- A7는 H, (C1-C6)알킬((C1-C6)alkyl), (C1-C6)플루오로알킬((C1-C6)fluoroalkyl), (C2-C6)알케닐((C2-C6)alkenyl), (C2-C6)알키닐((C2-C6)alkynyl) 또는 (C1-C6)알킬-ORa((C1-C6)alkyl-ORa)이며;- A8는 OH 또는 H이고;- 동일하거나 다른, Ra 및 Rb는 순수한 디아스테레오이소머(diastereoisomers) 및 디아스테레오이소머의 혼합물의 형상 및 카르보닐기 및 하이드록실기를 함유하는 화합물에 대하여 고리형 헤미케탈(cyclic hemiketal) 형상 또는 고리형 헤미아세탈(cyclic hemiacetal) 형상으로, H, (C1-C6)알킬((C1-C6)alkyl), (C1-C6)플루오로알킬((C1-C6)fluoroalkyl), (C1-C6)알킬-OH((C1-C6)alkyl-OH) 및 (C1-C6)알킬-O-(C1-C6)알킬((C1-C6)alkyl-O-(C1-C6)alkyl)으로 이루어진 그룹으로부터 선택되는, 화합물.