SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF A SERIES OF CAESPITIN DERIVATIVES
SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF A SERIES OF CAESPITIN DERIVATIVES
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DOI：
10.1128/aac.30.3.375
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发表时间：
1986-09-01
影响因子：
4.9
通讯作者：
SNYCKERS, FO
中科院分区：
文献类型：
--
作者：
VANDERSCHYF, CJ;DEKKER, TG;SNYCKERS, FO
本文介绍了天然间苯甲酮抗菌剂儿茶素的化学改性。这些修饰包括苯酮侧链的变化，在间苯甲酮核的4-位用异戊二烯基、烯丙基和苄基取代，以及通过醚化环化得到呋喃和苯并二氢吡喃化合物。这些衍生物中的几种显示出比儿茶素增强的体外效力。对这些化合物的微生物耐药性发展的研究表明，在代表性微生物菌株中，这些化合物经过几次传代后，没有或很少产生耐药性。
Chemical modification of the naturally occurring phlorophenone antimicrobial agent caespitin is described. These modifications include variations in the phenone side chain, substitution with prenyl, allyl, and benzyl in the 4-position of the phlorophenone nucleus, and ring cyclizations via etherification to give furan and chroman compounds. Several of these derivatives show enhanced in vitro potency over caespitin. Studies on the development of microbial resistance against these compounds show that no or very little resistance developed after several passes of these compounds in representative microbial strains.